Ontology highlight
ABSTRACT:
SUBMITTER: Tahirovic YA
PROVIDER: S-EPMC3142473 | biostudies-literature | 2008 Sep
REPOSITORIES: biostudies-literature
Tahirovic Yesim A YA Geballe Matthew M Gruszecka-Kowalik Ewa E Myers Scott J SJ Lyuboslavsky Polina P Le Phuong P French Adam A Irier Hasan H Choi Woo-Baeg WB Easterling Keith K Yuan Hongjie H Wilson Lawrence J LJ Kotloski Robert R McNamara James O JO Dingledine Raymond R Liotta Dennis C DC Traynelis Stephen F SF Snyder James P JP
Journal of medicinal chemistry 20080901 18
Enantiomeric propanolamines have been identified as a new class of NR2B-selective NMDA receptor antagonists. The most effective agents are biaryl structures, synthesized in six steps with overall yields ranging from 11-64%. The compounds are potent and selective inhibitors of NR2B-containing recombinant NMDA receptors with IC 50 values between 30-100 nM. Potency is strongly controlled by substitution on both rings and the centrally located amine nitrogen. SAR analysis suggests that well-balanced ...[more]